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An Absorption, Distribution, Metabolism, Excretion (ADME) Study of [14C]Subasumstat in Adults With Advanced or Metastatic Solid Tumors

Phase 1
Terminated
Conditions
Solid Tumors
Interventions
Registration Number
NCT05976334
Lead Sponsor
Takeda
Brief Summary

The main aim of this study is to assess how the human body of adults with advanced or metastatic solid tumors absorbs, distributes, metabolizes and excretes subasumstat following a single 1 hour infusion of subasumstat.

The study consists of two parts. In Part A, participants will receive a single infusion of C14 radiolabeled subasumstat. In Part B, participants will receive subasumstat treatment for up to 1 year.

Detailed Description

The drug being tested in this study is called \[14C\]subasumstat. \[14C\]Subasumstat is being tested to assess mass balance and absorption, distribution, metabolism, excretion (ADME) of people who have advanced or metastatic solid tumors.

The study will enroll approximately 10 patients. Participants will be enrolled to receive a single dose of \[14C\]subasumstat:

- \[14C\]Subasumstat 90 mg

Participants will be administered with a single dose of \[14C\]subasumstat 90 mg as a 1-hour intravenous (IV) infusion on Day 1 of Part A. All participants will be monitored for up to 14 days postdose. Participants will then have an option to enter Part B of the study to receive non-radiolabelled subasumstat 90 mg, IV infusion on Days 1, 4, 8, and 11 of a 21-day cycle for 3 cycles up to maximum treatment duration of 1 year.

This multi-center trial will be conducted in Hungary. The overall study duration is 12 months for Part A and 24 months for Part B.

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
3
Inclusion Criteria
  1. Participants have histologically or cytologically confirmed advanced (locally regionally recurrent not amenable to curative therapy) or metastatic solid tumors with no standard therapeutic option with a proven clinical benefit, are intolerant or have refused them.
  2. Participants have a performance status of 0 or 1 on the Eastern Cooperative Oncology Group Performance Scale.
  3. Participants demonstrate adequate organ function.
  4. Participants have recovered to Grade 1 or baseline from all toxicity associated with previous therapy or have the toxicity established as sequela.

Key

Exclusion Criteria
  1. Participants received treatment with radioisotopes within 5 half-lives before the first dose of the study drug.
  2. Participants received radiolabelled substances, were exposed to radiation sources within 12 months of the first dose in this study, or is likely to receive radiation exposure or radioisotopes within 12 months of the first dose in this study such that participation in this study would increase their total exposure beyond the recommended safe levels.
  3. Participants received extended field radiotherapy ≤4 weeks before the start of treatment.
  4. Participants have uncontrolled brain metastasis. Participants with treated brain metastases are allowed provided they are radiologically stable, without evidence of progression for at least 4 weeks by repeat imaging, clinically stable, and without requirement of steroid treatment for at least 14 days before first dose of study treatment.
  5. Participants had a second malignancy within the previous 3 years, except treated basal cell or localized squamous skin carcinomas, prostate cancer, cervical carcinoma in situ, resected colorectal adenomatous polyps, breast cancer in situ, or other malignancy for which the patient is not on active anticancer therapies.
  6. Major surgery ≤14 days from the first dose of study drug and not recovered fully from any complications from surgery.
  7. Baseline prolongation of the QT interval when corrected using Fridericia's formula (QTcF).
  8. Receiving or requires the continued use of medications that are known to be strong or moderate inhibitors and inducers of cytochrome P450 (CYP) 3A4/5 and strong P-glycoprotein (Pgp) inhibitors.
  9. Has active noninfectious pneumonitis or interstitial lung disease that required steroids.
  10. History of allogeneic tissue or solid organ transplant.
  11. Participants have active bacterial infection requiring systemic therapy <14 days before the start of treatment.
  12. Participants have an active HIV or any other relevant congenital or acquired immunodeficiency.
  13. Active hepatitis B, or hepatitis C infection.
  14. Any of the following uncontrolled heart diseases: congestive heart failure New York Heart Association Grade III or IV, unstable angina, myocardial infarction, unstable symptomatic ischemic heart disease, uncontrolled hypertension despite appropriate medical therapy, ongoing symptomatic cardiac arrhythmias >Grade 2, pulmonary embolism or symptomatic cerebrovascular events, or any other serious cardiac condition (eg, pericardial effusion or restrictive cardiomyopathy). Chronic atrial fibrillation on stable anticoagulant therapy is allowed.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
[14C] Subasumstat 90 mg[14C] SubasumstatParticipants will receive a single dose of \[14C\] Subasumstat 90 mg, IV infusion on Day 1 in Part A of the study. Following Part A, participants will have an option to receive subasumstat 90 mg, IV infusion on Days 1, 4, 8, and 11 of a 21 day cycle for 3 cycles followed by weekly maintenance dosing in Part B of the study up to maximum treatment duration of 1 year.
[14C] Subasumstat 90 mgSubasumstatParticipants will receive a single dose of \[14C\] Subasumstat 90 mg, IV infusion on Day 1 in Part A of the study. Following Part A, participants will have an option to receive subasumstat 90 mg, IV infusion on Days 1, 4, 8, and 11 of a 21 day cycle for 3 cycles followed by weekly maintenance dosing in Part B of the study up to maximum treatment duration of 1 year.
Primary Outcome Measures
NameTimeMethod
Cumulative Percentage of Urinary RecoveryUp to 14 days postdose

Cumulative amount of \[14C\]-radioactivity excreted in urine up to the last sampling interval.

Cumulative Percentage of Fecal RecoveryUp to 14 days postdose

Cumulative amount of \[14C\]-radioactivity excreted in feces up to the last sampling interval.

Cumulative Percentage of Combined RecoveryUp to 14 days postdose

Cumulative amount of \[14C\]-radioactivity excreted in urine, and feces up to the last sampling interval.

Percentage Of Recovered Total Radioactivity (TRA) In Urine And FecesUp to 14 days postdose

Percentage of recovered TRA in urine and feces for each interval over the entire period of collection will be reported.

Secondary Outcome Measures
NameTimeMethod
Cmax: Maximum Observed Plasma Concentration for Subasumstat and TRA in Plasma and Whole BloodPredose on Day 1 and at multiple time points postdose up to Day 14
Tmax: Time of First Occurrence of Cmax for Subasumstat and TRA in Plasma and Whole BloodPredose on Day 1 and at multiple time points postdose up to Day 14
AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Subasumstat and TRA in Plasma and Whole BloodPredose on Day 1 and at multiple time points postdose up to Day 14
Terminal Disposition Phase Half-life (T1/2z) for Subasumstat and TRA in Plasma and Whole Blood as Permitted by DataPredose on Day 1 and at multiple time points postdose up to Day 14
Clearance (CL) for Subasumstat and TRA in Plasma and Whole Blood as Permitted by DataPredose on Day 1 and at multiple time postdose points up to Day 14
Volume of Distribution at Steady-state (Vss) for Subasumstat and TRA in Plasma and Whole Blood as Permitted by DataPredose on Day 1 and at multiple time points postdose up to Day 14
Renal Clearance (CLR) for Subasumstat and TRA in UrinePredose on Day 1 and at multiple time points postdose up to Day 14
Number of Participants With One or More Serious Adverse Events (SAEs)From the start of study drug administration through 30 days after the last dose of study drug (up to approximately 1 year)

An AE is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. A SAE is defined as any untoward medical occurrence that at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of an existing hospitalization, results in persistent or significant disability or incapacity, is a congenital anomaly/birth defect or is a medically important event.

AUC∞: Area Under the Plasma Concentration-time Curve from Time 0 to Infinity for Subasumstat and TRA in Plasma and Whole Blood as Permitted by DataPredose on Day 1 and at multiple time points postdose up to Day 14
Cumulative Amount of Unchanged Subasumstat and TRA Excreted into the Urine (Aeurine)Predose on Day 1 and at multiple time points postdose up to Day 14
Number of Participants With Abnormal Electrocardiogram FindingsFrom the start of study drug administration through the last dose of study drug (up to approximately 1 year)

Abnormal laboratory values are those outside of normal range as assessed by the investigator.

Number of Participants With One or More Adverse Events (AEs)From the start of study drug administration through 30 days after the last dose of study drug (up to approximately 1 year)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment.

Number of Participants With Abnormal Laboratory ValuesFrom the start of study drug administration through the last dose of study drug (up to approximately 1 year)

Laboratory findings will include serum chemistry, hematology and urinalysis. Abnormal laboratory values are those outside of normal range as assessed by the investigator.

Relative Percentage of Circulatory Metabolites in PlasmaPredose on Day 1 and at multiple time points postdose up to Day 14
Relative Percentage Excretory Metabolites in UrinePredose on Day 1 and at multiple time points postdose up to Day 14
Relative Percentage Excretory Metabolites in FecesPredose on Day 1 and at multiple time points postdose up to Day 14

Trial Locations

Locations (2)

Central Hospital of Northern Pest - Military Hospital

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Budapest, Hungary

Pharmaceutical Research Associates Magyarorszag

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Budapest, Hungary

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